The present invention relates to a conjugate for individually dosing pharmaceutical preparations, a process for the production of such a conjugate as well as its use.
For a long time there has been a great demand to individually dose pharmaceutical preparations, i.e., accurately adapt their dose to a patient""s therapy course. This need is given particularly when chemotherapeutic agents are used. Many attempts have been made to achieve the above. However, the attempts have only showed little success by now.
Therefore, it is an object of the present invention to provide for individually dosing pharmaceutical preparations. According to the invention this is achieved by a conjugate which comprises an active substance and a compound having a binding site for metallic compounds.
The expression xe2x80x9cactive substancexe2x80x9d comprises substances of any kind which can be used for treating and/or diagnosing a disease, particularly a tumor, an infectious disease, skin disease and a disease of the immune system.
Examples of such substances include chemotherapeutic agents, e.g., antibiotics, virostatics, antiprotozoals and cytostatic agents. Examples of antibiotics include sulfonamides, tetracyclines, e.g., 7-chlorotetracycline, fusidic acid, gyrase inhibitors, e.g., quinolones, amphotericin, isoniazid, pyrazine 2-carboxylic acid, and pyrazinamide. Examples of virostatics include amantadine and rimantadine. Examples of antiprotozoals are mefloquine and primaquine. Examples of cytostatic agents are anthracyclines, e.g., doxorubicin, topoisomerase inhibitors, mitomycin A and C, bleomycinic acid, chlorambucil, melphalan and antifolates e.g., methotrexate. Furthermore such a substance may be an aminoanthraquinone such as celliton blue and acid black. Moreover, such a substance may be a photoactive substance, e.g., a porphyrin such as o-, m- and/or p-tetrahydroxyphenylporphine, o, m- and/or p-tetracarboxyphenylporphine and o-, m- and/or p-tetrasulfophenylporphine, a chlorin such as o-, m- and/or p-tetrabydroxyphenylchlorin, o-, m- and/or tetracarboxyphenylchlorin and o-, m- and/or p-tetrasulfophenylchlorin, or a bacteriochlorin, o-, m- and/or p-tetrahydroxyphenylbacteriochlorin such as o-, m- and/or p-tetracarboxyphenylbacteriochlorin, and o-, m- and/or p-tetrasulfophenylbacteriochlorin. In addition, such a substance may be a contrast medium for fluorospectroscopy, e.g., trifluoroacetic acid, nuclear resonance scanning or scintiscanning.
One or more of the above substances and/or analogues or derivatives thereof are present in a conjugate according to the invention. If several are present, they may be the same or differ from one another.
The expression xe2x80x9ccompound having a binding site for metallic compoundsxe2x80x9d includes compounds of any kind which have binding sites for metallic compounds. Examples of such binding sites include hydroxyl groups, particularly C-atoms bound hydroxyl groups, carbonyl and carboxyl groups. The compound may have one or more binding sites. The compound has preferably 2, more preferably 3 to 6, binding sites. If several binding sites are present, they may be the same or differ from one another. Examples of the above compounds are ethylenediaminetetraacetate (EDTA), diethylenetri-aminepentaacetate (DTPA), triethylenetetraminehexaacetate (TTHE), alizarin and derivatives thereof.
One or more of the above compounds are present in a conjugate according to the invention. If several are present, they may be the same or differ from one another. The presence of several of the above compounds supports the water solubility of the conjugate and its ability to bind metallic compounds.